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Brand Name :
AXS-07
Synonyms :
meloxicam/rizatriptan
Class :
Antimigraine Agents
Brand Name :
AXS-07
Synonyms :
meloxicam/rizatriptan
Class :
Antimigraine Agents
Safety and efficacy not established
Serious NSAID-related adverse effects on the heart, gastrointestinal tract, liver, and kidneys are more likely to occur in elderly persons. If therapy is required, take the smallest dose that works best for the shortest amount of time and keep an eye out for side effects
The nonsteroidal anti-inflammatory drug meloxicam produces beneficial actions as an anti-inflammatory agent with simultaneous pain-killing effects alongside fever reduction properties. The drug achieves its purpose by blocking the manufacturing process of specific chemicals named prostaglandins that take part in inflammatory activity. When levels of prostaglandin decrease through treatment with meloxicam medications can successfully handle pain and reduce inflammation and swelling.
The drug rizatriptan functions as a triptan medication that specifically interacts with serotonin (5-HT) receptors within the brain that activate the 5-HT1B and 5-HT1D receptors. When rizatriptan initiates activation of brain receptors it creates blood vessel constriction throughout the brain and decreases pain-related substance release for migraine symptom relief.
People use meloxicam mainly to treat symptoms of rheumatoid arthritis as well as osteoarthritis and juvenile rheumatoid arthritis.
The medication rizatriptan functions to treat acute migraines for adult patients. The medication has no role in prevention against migraines or alternative headache symptoms.
Dizziness
Somnolence
The CV Risk includes elevated heart attack and stroke probabilities while CABG surgery requires strict avoidance of the medication. The GI risk includes severe bleeding together with ulcers and perforation and both age groups together with gastrointestinal disease history are at elevated risk.
Contraindication
meloxicam:
• Allergy or hypersensitivity
• Asthma, nasal polyps, and allergic reactions
• Active gastrointestinal bleeding or peptic ulcers
• Severe liver or kidney disease
• Third trimester of pregnancy
rizatriptan:
• Allergy or hypersensitivity
• Ischemic heart disease
• Uncontrolled hypertension
• Severe liver impairment
Caution
meloxicam:
• Cardiovascular risk
• Gastrointestinal effects
• Asthma
• Skin reactions
Pregnancy consideration:
US FDA pregnancy category: Not assigned.
Lactation:
Excreted into human milk: Not known.
Pregnancy category:
• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
• Category N: There is no data available for the drug under this category
The nonsteroidal anti-inflammatory drug (NSAID) known as meloxicam exhibits anti-inflammatory and antipyretic along with analgesic properties. Select COX-2 inhibition through the pain-killing effects of meloxicam leads to reduced formation of inflammatory prostaglandins in the body. When prostaglandin synthesis gets inhibited through meloxicam treatment the medication effectively reduces pain alongside inflammation and swelling especially when treating arthritis cases. Stimulation of these receptors through rizatriptan leads to cranial blood vessel constriction and inhibits pro-inflammatory neuropeptides release. The therapeutic mechanism of this medication helps patients cope with their migraine symptoms which specifically includes nausea and headache pain and light and sound sensitivities.
Pharmacodynamics:
The pain and inflammation medication meloxicam functions as an NSAID that principally blocks COX-2 activity which controls prostaglandin formation in the body. When taken the medication triggers pain reduction together with swelling relief while also enhancing joint movement abilities. However, the COX-1 inhibitor properties of this drug could impact protection mechanisms in the stomach and kidneys. Through its function as a selective serotonin receptor agonist (5-HT1B/1D) Rizatriptan tightens blood vessels in the cranial area which reduces migraine-related vessel dilation and minimizes throbbing pain. its ability to control pro-inflammatory neuropeptide release aids in the relief of nausea vomiting along with sensitivity to light/sound and vomiting. The medication exclusively treats migraines without impact against other headache types.
Pharmacokinetics:
Absorption
Meloxicam: Rapid absorption with peak plasma concentration at 0.88 hr (faster than meloxicam alone: 4–5 hr).
Rizatriptan achieves its highest plasma levels at 0.75 hours after administration.
Distribution
The body protein binds approximately 99.4% of meloxicam and its volume of distribution (Vd) reaches 10 L. The drug-binding element for Rizatriptan is proteins at 14% but its volume distribution shows 140 L in males and 110 L in females.
Metabolism
The liver metabolism of meloxicam produces four inactive metabolic products through a widespread metabolic process.
The liver performs extensive drug metabolism to transform meloxicam through CYP2C9 metabolic enzymes and a lesser amount occurs through CYP3A4 enzyme action. As a result, the body breaks down meloxicam into 5′-carboxy meloxicam comprising 60% of dose alongside 9% becoming 5′-hydroxymethyl meloxicam.
The peroxidase enzyme generates multiple metabolites from the drug substance that represent 16% and 4% of the administered dose.
The main route of processing Rizatriptan involves monoamine oxidase-A enzymes that create the inactive compound indole acetic acid.
Minor active metabolite: N-monodesmethyl-rizatriptan (14% of parent compound, similar elimination rate).
The remaining metabolites are inactive and include N-oxide together with 6-hydroxy compound as well as sulfate conjugate of 6-hydroxy metabolite.
Elimination and Excretion
Meloxicam:
Half-life: 18 hr
Clearance: 7–9 mL/min
Excretion: Equally through urine and feces as metabolites.
Rizatriptan:
Half-life: 2 hr
Excretion: Urine (12%), Feces (82%).
The tablet is taken orally and may take with or without food.
Patient information leaflet
Generic Name: meloxicam/rizatriptan
Why do we use meloxicam/rizatriptan?
Acute treatment of migraine (with or without aura) in adults
This medication delivers quick pain relief and helps decrease symptoms including nausea and vomiting as well as sensitivity to light and sound during migraines.
The combination of meloxicam anti-inflammatory and analgesic effects and rizatriptan vasoconstrictive actions provides joint pain treatment.
The substance provides continuous migraine treatment for 24–48 hours which enables patients to avoid additional rescue medications.
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